Asymmetric oxy-Michael addition to γ-hydroxy-α,β-unsaturated carbonyls using formaldehyde as an oxygen-centered nucleophile

Org Lett. 2014 Dec 5;16(23):6264-6. doi: 10.1021/ol503104b. Epub 2014 Nov 10.

Abstract

Formaldehyde was utilized as an oxygen-centered nucleophile in an asymmetric oxy-Michael addition to γ-hydroxy-α,β-unsaturated carbonyl compounds using bifunctional organocatalysts through hemiacetal intermediates. The cyclic acetal product could be further transformed into β-hydroxycarbonyl compounds, useful synthetic intermediates leading to various important target molecules. As such, this method is an example of a novel formal asymmetric hydration of α,β-unsaturated carbonyl compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetals / chemical synthesis
  • Acetals / chemistry
  • Catalysis
  • Formaldehyde / chemistry*
  • Ketones / chemistry*
  • Molecular Structure
  • Oxygen / chemistry*
  • Stereoisomerism

Substances

  • Acetals
  • Ketones
  • Formaldehyde
  • Oxygen